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Assay Detail

CHEMBL5500912

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant SIRT2 (unknown origin) deacetylase activity using Ac-RHKK(Ac)-MCA as substrate incubated for 60 mins in presence of NAD by fluorogenic assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

NAD-dependent protein deacetylase sirtuin-2 (CHEMBL4462)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Ligand-based design and synthesis of new trityl histamine and trityl cysteamine derivatives as SIRT2 inhibitors for cancer therapy.
Badran MM, Abbas SH, Tateishi H, Maemoto Y, Toma T, Ito A, Fujita M, Otsuka M, Abdel-Aziz M, Radwan MO.
Eur J Med Chem (2024) 269 : 116302 -116302
PubMed 38484678 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.02 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770903 1 6.92
CHEMBL5555254 1 5.25
CHEMBL5518043 1 5.12
CHEMBL5556453 1 5.06
CHEMBL5557521 1 5.06
CHEMBL5542326 1 5.00
CHEMBL5557139 1 4.97
CHEMBL5559510 1 4.92
CHEMBL5542871 1 4.91
CHEMBL5557325 1 4.85
CHEMBL5505900 1 4.81
CHEMBL5556326 1 4.58
CHEMBL5558060 1 4.56
CHEMBL5527915 1 4.30
CHEMBL5523388 1 -
CHEMBL5557313 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770903 IC50 = 120.0 nM 6.92
CHEMBL5555254 IC50 = 5630.0 nM 5.25
CHEMBL5518043 IC50 = 7610.0 nM 5.12
CHEMBL5556453 IC50 = 8620.0 nM 5.06
CHEMBL5557521 IC50 = 8630.0 nM 5.06
CHEMBL5542326 IC50 = 9910.0 nM 5.00
CHEMBL5557139 IC50 = 10610.0 nM 4.97
CHEMBL5559510 IC50 = 12020.0 nM 4.92
CHEMBL5542871 IC50 = 12420.0 nM 4.91
CHEMBL5557325 IC50 = 14180.0 nM 4.85
CHEMBL5505900 IC50 = 15380.0 nM 4.81
CHEMBL5556326 IC50 = 26140.0 nM 4.58
CHEMBL5558060 IC50 = 27280.0 nM 4.56
CHEMBL5527915 IC50 = 49640.0 nM 4.30
CHEMBL5523388 IC50 > 50000.0 nM -
CHEMBL5557313 IC50 > 50000.0 nM -